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JP6670223B2 |
The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capabl...
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JP6664408B2 |
The invention relates to compounds of formula (I), to the pharmaceutical compositions comprising same, and to the use thereof in the treatment of bacterial, fungal, viral and parasitic infections or in the treatment of cancer in humans o...
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JP6621217B2 |
Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using ...
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JP6608929B2 |
Described herein, inter alia, are compositions and methods for treating or preventing hyperproliferative disorders, including cancer.
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JP6604938B2 |
The present invention provides haloalkane substrates, and linkers for connecting such substrates to functional elements (e.g., tags, labels, surfaces, etc.). Substrates and linkers described herein find use, for example, in labeling, det...
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JP6578277B2 |
Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1a and R1b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. T...
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JP6542127B2 |
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorde...
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JP2019059781A |
To provide amino steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal, and compositions containing these amino steroid compounds.This application is directed to various amino steroid compounds for the inhibition...
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JP2019048851A |
To provide modified drugs for use in liposomal nanoparticles.Provided herein is a drug derivative suitable for loading into liposomal nanoparticle (LN) carriers. In some preferred aspects, the derivative comprises a drug with low water s...
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JP2019011345A |
To provide a lipid-therapeutic nucleic acid composition, encapsulating nucleic acid at high efficiency, high in a ratio of pharmaceutical:lipid, protecting the encapsulated nucleic acid from degradation and clarification in serum, suitab...
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JP6449274B2 |
Various prodrug compounds having the general structure: Active agent—(acid)-(linker)—SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.
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JP6437636B2 |
The present invention provides amphiphilic compounds with a tetradecahydrophenanthrene skeleton of formula (I), wherein R1-R5 are as defined herein, and their enantiomers, exhibiting neuroprotective effects, for use as medicaments for tr...
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JP2018188472A |
To develop a novel compound which can be delivered effectively and efficiently to a site of action in a certain state (e.g., disease) for preventing, reducing, or treating the state in a biological subject while minimizing side effects.T...
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JP2018528944A |
Methods and systems for making intermediates in the synthesis of onapristones are provided. Aspects include optical conversion of onapriston synthetic intermediates using a narrowband frequency light source.
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JP2018138594A |
To provide polymorphic forms of onapristone and methods of making and using such polymorphic forms.Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties. Methods of making poly...
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JP6272224B2 |
A hydrogel polymer includes a ceragenin compound. The ceragenin compound has a hydrophobicity/hydrophilicity that produces a release rate in a range of 0.1-100 μg/ml for at least 3 days.
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JP2017535570A |
The present invention relates to compounds of formula (IA) and formula (IB) for treating TGR5-mediated diseases or conditions and pharmaceutically acceptable salts thereof (in formula, R).1, R2, R3, R4, R5, R6, R7, R8, R9And m are as def...
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JP2017533923A |
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing these compounds and methods of using these compounds to treat TGR5-mediated diseases or condi...
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JP6222057B2 |
A chemically amplified resist composition comprising a base polymer, an acid generator, and a basic compound which is a cholanoate having an acid labile group-protected amino group has a high contrast of alkaline dissolution rate before ...
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JP6157492B2 |
The present invention relates to a process for the preparation of sterol derivatives comprising the reaction of an α-epoxy compound with an amine in an alcohol comprising 3 to 5 carbon atoms as a solvent.
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JP6127982B2 |
A problem of the present invention is to provide a liquid crystal aligning agent which never deteriorates even in a method where UV is irradiated such as a liquid crystal dropping method or the like, and is capable of forming a liquid cr...
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JP2017039649A |
To provide Fusarium head blight mycotoxin inhibiting agents and methods.The present invention provides Fusarium head blight mycotoxin inhibiting agents comprising at least one of a compound represented by formula (1) and pharmaceutically...
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JP2017019857A |
To provide novel compounds.Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to f...
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JP2016222671A |
To provide methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a human subject, and to provide compounds that yield or generate 3APS, either in vitro or in vivo.This invention relates to ...
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JP5992019B2 |
Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitate...
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JP5872897B2 |
The present invention relates to novel chemical compounds, in particular cholest-4-en-3-one oxime derivatives and to the use thereof as medicaments, especially as cytoprotective medicaments, in particular neuroprotective, cardioprotectiv...
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JP2016505038A |
The present invention is a novel compound and composition of 11β-hydroxysteroids, as well as pharmaceuticals for preventing or reversing mitochondrial damage in human or animal subjects, for treating or preventing diseases associated wi...
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JP5865845B2 |
The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonizing effect and processes for their preparation, their use for the treatment and/or prophylaxis o...
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JP2016006068A |
To provide a biocompatible conjugated polymer nanoparticle.The invention relates to a biocompatible conjugated polymer nanoparticle comprising a copolymer backbone, a plurality of side-chains covalently linked to the backbone and a plura...
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JP5828159B2 |
This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and...
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JP2015205899A |
To provide novel medicaments which are useful as cytoprotective medicaments, in particular as neuroprotective, cardioprotective and/or hepatoprotective medicaments which can inhibit and/or treat cell death necrosis and/or pathological ap...
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JP2015532263A |
Provided are a novel crystalline polymorph of uripristal acetate, which is useful as a preventive and / or therapeutic agent for uterine fibroids, a contraceptive, and the like, and a method for producing the same. Crystallization or tra...
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JP5770235B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP5663303B2 |
This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and...
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JP2014532077A |
The present invention relates to novel aminosteroid derivatives substituted at the 3 and / or 6 positions and relates to their use in the treatment of type 2 diabetes and insulin resistance.
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JP5564490B2 |
wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compo...
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JP5452932B2 |
New and known 4-cholesten-3-one oxime derivatives (I) are used as medicaments. 4-Cholesten-3-one oxime derivatives of formula (I) and their acid addition salts are used as medicaments. X = O or NOH; R = (CH 2) 4CH(Me) 2, (CH 2) 3CH=C(Me)...
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JP5419750B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP5417562B2 |
The invention provides 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienediones as antiprogestational agents.
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JP5399711B2 |
The invention relates to a new process for the synthesis of high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention...
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JP5386362B2 |
Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treat...
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JP5274453B2 |
A new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpreg
na-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. Th...
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JP5276020B2 |
The present invention provides a novel series of cationic, lipid-based, 17α-substituted-estradiol derivatives. The present invention further provides a process for the preparation of a novel series of 17α-substituted-estradiol derivati...
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JP5261481B2 |
The present invention relates to a process for the synthesis of the 17-acetoxy-11β-[4-(dimethylamino)-phenyl]-21-methoxy-19-nor
pregna-4,9-dien-3,20-dione of formula (I): from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of...
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JP5230450B2 |
The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.
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JP5229700B2 |
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JP5216782B2 |
The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx (I) wherein R is the corticosteroid residue of formula (II): wherein:...
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JP2013514338A |
The present invention relates to a compound of formula (I) for its use for reversing or inhibiting multidrug resistance.
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JP5191079B2 |
There is provided a compound of Formula I wherein X is a ring system; R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R 2 is any one of a sulphamate group, a...
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JP2013506686A |
The present disclosure relates to methods for the modulation of autophagy and the treatment of autophgy-related diseases, including cancer, neurodegenerative diseases and pancreatitis.
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